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1. 发明申请

WO0218946A3 IMMOBILISED PHOSPHATIDIC ACID PROBE 审中-公开
标题翻译：固定化磷酸探针
公开(公告)号：WO0218946A3
公开(公告)日：2002-10-24
申请号：PCT/GB0103791
申请日：2001-08-23
申请人： BABRAHAM INST , UNIV CAMBRIDGE TECH , STEPHENS LEN , HAWKINS PHILLIP THOMAS , HOLMES ANDREW BRUCE , MANIFAVA MARIA , LIM ZE YI , KTISTAKIS NICHOLAS , THURING JOHANNES WILHELMUS JOH
发明人： STEPHENS LEN , HAWKINS PHILLIP THOMAS , HOLMES ANDREW BRUCE , MANIFAVA MARIA , KTISTAKIS NICHOLAS , THURING JOHANNES WILHELMUS JOH
IPC分类号： G01N33/543 , G01N33/68 , G01N33/53
CPC分类号： G01N33/54353 , G01N33/68
摘要： Probes comprising an immobilised Phosphatidic Acid attached onto a solid support are described, for example, as shown in formula (I) and (V): (a) the linker consists of aryl, heteroaryl, alkyl with possible heteroatoms and/or unsaturations, preferably chains of (CH2)n, with n = 8-20, most preferably n = 11; (b) the heteroatom X maybe O, S, or most preferably NH; (c) the functional group (FG) is a carbonyl from a carboxylate (thiolo)ester, or, most preferably an amide; (d) the R-substituent carries an aryl, alkyl group, or a combination, preferably R=CmH2m+1, m = 8-20, m = 16 optimal; (e) the ion M represents any cation, preferably Na , NH4+; (f) unsaturations are allowed, such as in an arachidonyl side chain and (g) = solid support with attachment to functional group. where: R = aryl, alkyl group, or a combination, preferably R = CmH2m+1, m = 8-20, m = 16 is optimal. R3 is P(O)(OM)2; R5 = H(PI(3)P); R3 = H; R4 = P(O)(OM)2; R5 = H(PI(4)P); R3 = H; R4 = H; R5 = P(O)(OM)2 (PI(5)P); R3 = P(O)(OM)2; R4 = P(O)(OM)2; R5 = H(PI(3,4)P2); R3 = P(O)(OM)2; R4 = H; R5 = P(O)(OM)2 (PI(3,5)P2); R3 = H; R4 = P(O)(OM)2; R5 = P(O)(OM)2 (PI(4,5)P2); or R3 = P(O)(OM)2; R4 = P(O)(OM)2; R5 P(O)(OM)2 (PI(3,4,5)P3). M = any cation, preferably Na , NH4 *Denotes a stereogenic centre. More preferably a stereogenic centre with an R absolute configuration. Linker = aryl, heteroaryl, alkyl with possible heteroatoms and/or unsaturations. Preferably chains of (CH2)n with n = 8-20, most preferably n = 11. X = O, S, or, most preferably NH. FG = Carbonyl from a carboxylate, thiolo(ester), or, most preferably an amide. Unsaturations are allowed, such as in an arachidonyl side chain. = solid support with attachment to functional group. Use of the probes to identify Phosphatidic Acid binding protein or phosphoinositide binding proteins is also described.
摘要翻译：例如，如式（I）和（V）所示，包含固定在固体载体上的固定化磷脂酸的探针：（a）连接体由芳基，杂芳基，可能的杂原子和/或不饱和基团（CH 2）n的链，n = 8-20，最优选n = 11; （b）杂原子X可以是O，S，或最优选NH; （c）官能团（FG）是羧酸酯（thiolo）酯的羰基，或最优选酰胺; （d）R取代基带有芳基，烷基或组合，优选R = CmH2m + 1，m = 8-20，m = 16最优; （e）离子M表示任何阳离子，优选Na +，NH 4 +; （f）允许不饱和度，例如在花生四烯酰侧链中，（g）=与官能团连接的固体支持物。其中：R =芳基，烷基或组合，优选R = CmH2m + 1，m = 8-20，m = 16是最佳的。 R3是P（O）（OM）2; R5 = H（PI（3）P）; R3 = H; R4 = P（O）（OM）2; R5 = H（PI（4）P）; R3 = H; R4 = H; R5 = P（O）（OM）2（PI（5）P）; R3 = P（O）（OM）2; R4 = P（O）（OM）2; R5 = H（PI（3,4）P2）; R3 = P（O）（OM）2; R4 = H; R5 = P（O）（OM）2（PI（3,5）P2）; R3 = H; R4 = P（O）（OM）2; R5 = P（O）（OM）2（PI（4,5）P2）; 或R3 = P（O）（OM）2; R4 = P（O）（OM）2; R5 P（O）（OM）2（PI（3,4,5）P3）。 M =任何阳离子，优选Na +，NH 4 + *表示立体中心。更优选具有R绝对构型的立体中心。连接子=芳基，杂芳基，具有可能的杂原子和/或不饱和基团的烷基。优选（CH 2）n的链，n = 8-20，最优选n = 11.X = O，S，或最优选NH。 FG =羧酸羰基，硫代（酯），或最优选酰胺。允许不饱和度，例如在花生四烯酸侧链中。 =与功能基团相连的固体支持物。还描述了使用探针来鉴定磷脂酸结合蛋白或磷酸肌醇结合蛋白。

2. 发明申请

WO2007031440A3 2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES 审中-公开
标题翻译： 2-苯胺-4-芳基取代的噻唑衍生物
公开(公告)号：WO2007031440A3
公开(公告)日：2007-08-02
申请号：PCT/EP2006066015
申请日：2006-09-05
申请人： JANSSEN PHARMACEUTICA NV , THURING JOHANNES WILHELMUS JOH , MACDONALD GREGOR JAMES , GRANTHAM CHRISTOPHER JAMES , DINKLO THEODORUS , LESAGE ANNE SIMONE JOSEPHINE
发明人： THURING JOHANNES WILHELMUS JOH , MACDONALD GREGOR JAMES , GRANTHAM CHRISTOPHER JAMES , DINKLO THEODORUS , LESAGE ANNE SIMONE JOSEPHINE
IPC分类号： C07D277/42 , A61K31/426 , A61K31/427 , A61K31/4436 , A61P25/18 , A61P25/28 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
CPC分类号： C07D471/04 , C07D277/42 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention concerns the use of a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C 1-6 alkyl, Het 1 , HO-C 1-6 alkyl-, cyano-C 1-6 alkyl-, amino-C(=O)-C 1-6 alkyl-, formylamino-C 1-6 alkyl-, C 1-6 alkyl-C(=O)-NH-C 1-6 alkyl-, mono- or di(C 1-6 alkyl)amino-C(=O)-C 1-6 alkyl-, phenyl-C 1-6 alkyl-, or He 4 -C 1-6 alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C 1-6 alkyl, C 1-6 alkyl -O-, C 1-6 alkyl, Ar or polyhaloC 1-6 alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C 1-6 alkyl or C 1-6 alkyl-O-; Het 1 represents morpholinyl; pyrazolyl or imidazolyl; Het 4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C 1-6 alkyl, C 1-6 alkyl-O- or polyhaloC 1-6 alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the a7 nicotinic receptor is beneficial.
摘要翻译：本发明涉及式（I）化合物，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式的用途，其中Z是氢，卤素，C 1-6 - 烷基，Het 1，HO-C 1-6烷基 - ，氰基-C 1-6烷基 - ，氨基-C （= O）-C 1-6烷基 - ，甲酰氨基-C 1-6烷基 - ，C 1-6烷基-C（C 1 -C 6烷基） = O）-NH-C 1-6烷基 - ，单 - 或二（C 1-6烷基）氨基-C（= O）-C≡N 1-6烷基 - ，苯基-C 1-6烷基 - 或He + 4 -C 1-6烷基 - ; Q是苯基，吡啶基，苯并呋喃基，2,3-二氢 - 苯并呋喃基，吡唑基，异恶唑基或吲唑基，其中每个所述环系统任选被至多三个各自独立地选自卤素，氰基，C1- C 1-6烷基，C 1-6烷基-O-，C 1-6烷基，Ar或多卤代C 1-6烷基 ; L是苯基，吡啶基，嘧啶基，8-氮杂嘧啶基，哒嗪基，咪唑并噻唑基或呋喃基，其中每个所述环系可以任选被一个或两个或多个取代基取代，每个取代基独立地选自卤素，羟基，氨基，氰基，C 1-6烷基或C 1-6烷基-O-; Het 1表示吗啉基; 吡唑基或咪唑基; Het 4表示吗啉基，吡唑基或咪唑基; Ar代表任选被卤素取代的苯基，C 1-6烷基，C 1-6烷基-O-或多卤代C 1-6烷基; 用于制造用于预防或治疗或预防精神障碍，智力损伤障碍或调节α7烟碱受体有益的疾病或病症的药物。

3. 发明专利

AU8232301A Immobilised phosphatidic acid probe 未知
公开(公告)号：AU8232301A
公开(公告)日：2002-03-13
申请号：AU8232301
申请日：2001-08-23
申请人： BABRAHAM INST , UNIV CAMBRIDGE TECH
发明人： HAWKINS PHILLIP THOMAS , HOLMES ANDREW BRUCE , MANIFAVA MARIA , KTISTAKIS NICHOLAS , THURING JOHANNES WILHELMUS JOH
IPC分类号： G01N33/543 , G01N33/68 , G01N33/53

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